Disease relevance of Lofexidine

• Hemodynamic effect of lofexidine with a diuretic in hypertension [1].
• Clonidine and lofexidine appear equally effective for inpatient settings, but the lower incidence of hypotension makes lofexidine more suited to use in outpatient settings [2].
• The effectiveness of lofexidine is comparable to that of clonidine, but lofexidine has a lower incidence of toxicity [3].
• Tic severity decreased by 27% in the lofexidine group, compared to 0% in the placebo group [4].
• METHODS: A randomized placebo-controlled parallel group trial was undertaken in the University Hospital Gynaecology Clinic. Women with pelvic pain of at least 6 months duration were eligible, and were randomized using a sealed envelope system to receive up to 600 mg lofexidine hydrochloride twice daily over 8 weeks or placebo [5].

Psychiatry related information on Lofexidine

• Lofexidine is used clinically for treating opiate withdrawal symptoms and yohimbine induces stress-like responses in humans and non-humans [6].
• Lofexidine in hyperactive and impulsive children with autistic disorder [7].
• Subjects from a specialty tic disorders clinic were randomly assigned to receive 8 weeks of treatment with lofexidine or placebo under double-blind conditions [4].
• Currently, the main treatments for opiate dependence in China include short-term detoxification with opiate agonists or non-opiate agents, such as clonidine or lofexidine; Chinese herbal medicine and traditional non-medication treatments are also used [8].
• Only one lofexidine recipient was prematurely interrupted, due to transient hallucinations [9].

High impact information on Lofexidine

• We measured the first dosage effect and the long-term effect of lofexidine on blood pressure, heart rate, plasma catecholamines, and their major metabolites in 16 patients with primary hypertension who were receiving 50 mg hydrochlorothiazide twice a day while they were recumbent and upright and during isometric handgrip contraction [1].
• We also measured the first dosage effect of lofexidine on forearm blood flow and its long-term effect on plasma renin activity [1].
• Results suggested that reduction of blood pressure by lofexidine depended on lack of increase in TPR in response to reduction of cardiac output; the hemodynamic pattern of this centrally acting adrenergic blocker closely resembled that reported for beta blockers [10].
• This study evaluated the efficacy and safety of Lofexidine in treating children with tic disorders and attention deficit hyperactivity disorder (ADHD) [4].
• On the Continuous Performance Test, commission errors decreased by 25% and omission errors by 20% in the lofexidine group, compared with increases of 33% in commission errors and of 36% in omission errors in the placebo group [4].

Chemical compound and disease context of Lofexidine

• The comparative efficacy and safety of lofexidine and clonidine in patients with mild to moderate systemic hypertension were evaluated [3].
• An accelerated 5-day lofexidine regimen may attenuate opiate withdrawal symptoms more rapidly than conventional 10-day lofexidine or methadone treatment schedules without exacerbating hypotensive side effects [11].
• FINDINGS: Substitute methadone for opiate addiction, substitute benzodiazepines for benzodiazepine-dependent patients, lofexidine for opiate detoxification, naltrexone for opiate relapse prevention and acamprosate for alcohol relapse prevention were widely acceptable and available interventions [12].

Biological context of Lofexidine

• There was a positive correlation between the decrease in blood pressure induced by single doses and by long-term dosing, which suggests that lofexidine in a single dosage at the start of therapy may facilitate identification of responders [1].
• Lofexidine did not prevent or diminish the pressure and heart rate rise by isometric handgrip contractions [1].
• Biotransformation of lofexidine in humans [13].
• Effects of lofexidine, an alpha 2-adrenoreceptor agonist, on ocular blood flow and ion transport of rabbit iris-ciliary body [14].
• The effect of topical unilateral application of lofexidine, an alpha 2-agonist, on ocular regional blood flow was tested in anesthetized rabbits using radiolabeled microspheres [14].

Anatomical context of Lofexidine

• Drugs such as clonidine, methyldopa, guanabenz, guanfacine, and lofexidine have their primary site of antihypertensive action in the central nervous system (CNS) to activate alpha 2-adrenergic receptors and lower arterial pressure [15].
• Actions of lofexidine on isolated heart and smooth muscle preparations [16].
• A significant reduction in blood flow was found only in the ciliary body of the treated eye at 1 hr after lofexidine treatment [14].

Associations of Lofexidine with other chemical compounds

• In dialy dosages of 0.2 or 0.4 mg, monotherapy with lofexidine produced significant decreases in blood pressure and heart rate that were not different from those with clonidine [17].
• This study compares the clinical responses to methadone and lofexidine in the treatment of opiate withdrawal in 86 polydrug-abusing opiate addicts, using a randomised double-blind study design [18].
• 2-[1-(2,6-Dichlorphenoxy)-ethyl]-2-imidazoline hydrochloride (lofexidine, Lofetensin and Loxacor) elicited no evidence of teratogenicity when administered orally during the period of organogenesis to pregnant rats at doses up to 3.0 mg/kg/day or to pregnant rabbits at doses up to 15.0 mg/kg/day [19].
• In rabbits and guinea pigs, lofexidine exhibited local anaesthetic effects and its potency and duration of action were comparable to those of the reference compounds (tetracaine or mepivacaine) [20].

Gene context of Lofexidine

• After control of blood pressure with lofexidine (a centrally acting imidazoline derivative), plasma beta thromboglobulin levels decreased in 9 of the 10 hypertensive patients, but increased in one who showed no change in blood pressure [21].

Analytical, diagnostic and therapeutic context of Lofexidine

• In addition, lofexidine did not have a consistent effect on speedball self-administration and extinction behavior [22].
• Animal experiments on the safety pharmacology of lofexidine [20].
• Five published reports of clinical trials of lofexidine have been identified from peer-reviewed journals in the eight years between 1990 and 1998--all published within the last three years [23].
• Lofexidine was applied in a control group of 48 addicts [24].

References